聚山梨醇-80修饰的神经毒素纳米粒经大鼠鼻腔给药后体内分布研究  

Distribution in mouse tissues of P-80 modified neurotoxin nanoparticles after intranasal administration in rats

作　　者：周荣[1] 金铭[1] 沈淼山 阮叶萍[1] 

机构地区：[1]浙江中医药大学,浙江杭州310053

出　　处：《中草药》2015年第17期2599-2602,共4页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年科学基金项目(81102842)

摘　　要：目的制备异硫氰酸荧光素(FITC)标记的经聚山梨醇-80(P-80)修饰的神经毒素纳米粒(P-80-NT-NP),分析其经鼻腔给药后在大鼠体内组织分布规律。方法制备FITC标记的P-80-NT-NP和神经毒素纳米粒(NT-NP),经大鼠鼻腔给药后,于5、15、30、60、120、240 min采集血样,采集脑、心、肝、脾、肺、肾组织样品,以FITC标记的神经毒素(FITC-NT)为指标成分,采用荧光分光光度计分析手段,考察NT-NP经P-80修饰前后药物在大鼠体内各组织中分布状况的差异。结果P-80-NT-NP和NT-NP经鼻腔黏膜给药后5、15、30、60、120、240 min,药物在血浆、心、肝、脾、肺、肾和脑中均有分布,其中以肝组织中分布最高,肾组织其次。给药后120 min P-80-NT-NP给药组血浆、脑中NT的质量浓度高于NT-NP组,而在肝组织中低于NT-NP组,差异均显著(P<0.05)。结论 P-80可有效增加NT-NP经鼻腔吸收入脑的药量,为脑靶向制剂的进一步开发应用提供依据。Objective To prepare neurotoxin nanoparticles（NT-NP） labeled by FITC and modified by polysorbate-80（P-80）, and to compare the in vivo tissue distribution after intranasal administration in rat. Methods The FITC labeled P-80-NT-NP and NT-NP were prepared, blood samples were collected after intranasal administration in rats at 5, 15, 30, 60, 120, and 240 min, and the brain, heart, liver, spleen, lung, kidney tissue samples were collected. Using FITC-NT as the index component and fluorescence analysis method, the differences of the nanoparticles distribution in rats tissues after modified by P-80 were investigated. Results After 5, 15, 30, 60, 120, and 240 min of intranasal administration of P-80-NT-NP and NT-NP, the drug was distributed in plasma, heart, liver, spleen, lung, kidney, and brain. After 120 min of administration, the NT concentration in plasma and brain of P-80-NT-NP group was higher than that of NT-NP group, while the NT concentration in liver was lower than that in NT-NP group, with significant difference. Conclusion P-80 can effectively increase the nasal absorption of NT-NP into the brain and other tissues, which provides the basis for further development and application of preparation of the drug targeting to brain.

关 键 词：神经毒素 纳米粒 异硫氰酸荧光素标记 体内分布 鼻腔给药 聚山梨醇-80 

分 类 号：R285.5[医药卫生—中药学]